Development and characterization of an oral dosage form containing Entacapone, Carbidopa, and L-dopa

Resumo

Entacapone is a catechol-o-methyltransferase (COMT) inhibitor used in association with carbidopa and L-dopa in the treatment of Parkinson’s disease. The tablets containing entacapone associated with carbidopa and L-dopa should also contain elements to promote its bioavailability, since entacapone presents low solubility and low permeability. The objectives of this study were the development and physicochemical characterization of tablets containing an association of entacapone, carbidopa, and L-dopa using Stalevo® as a reference medication. To achieve these goals, different batches of tablets were produced containing surfactants such as sodium dodecyl sulfate and poloxamers 118 and 407 using the wet granulation method in a high shear mixer. The tablet cores obtained were approved regarding the following physicochemical properties: friability, hardness, disintegration, content of active ingredient, and dissolution. The coated tablets containing poloxamer 407 presented dissolution profile similar to the reference medication.

Descrição

Palavras-chave

Levodopa, Doença de Parkinson, Carbidopa, Entacapone, Poloxamer, Tecnologia farmacêutica, Levodopa, Parkinson disease, Carbidopa, Pharmaceutical Technology, Entacapone, Poloxamer

Citação

Rodovalho-Mitani, Luciana Ferreira Fonseca et al. Development and characterization of an oral dosage form containing Entacapone, Carbidopa, and L-dopa. Revista Brasileira de Farmácia, Rio de Janeiro, v. 95, n. 3, p. 796-813, 2014.